Effects of in-vitro activity of miconazole and ketoconazole in phospholipid formulations.
Antifungal agents are often used in liposomal formulations in order to improve their pharmacological activity, but how vesicle inclusion can actually affect this is still not fully understood. We report here the results obtained from evaluation of the in-vitro activity against Candida albicans ATCC E10231 of miconazole and ketoconazole in various vesicular and non-vesicular preparations, obtained from egg and soya phospholipids, using time-kill curves. In most cases inclusion of miconazole or ketoconazole in liposomes led to a delayed and decreased activity of the drugs, with detectable differences among the various phospholipid concentrations and different liposomal preparations (small unilamellar vesicle, liposomes, multilamellar aggregates and broken liposomal structures). The results obtained may be helpful in the study of new preparations of antifungal agents entrapped in liposomal structures.
De Logu
A
A
Dipartimento di Scienze Chirurgiche e Trapianti d'Organo, Università degli Studi di Cagliari, Italy. adelogu@vaxca1.unica.it
Fadda
A M
AM
Anchisi
C
C
Maccioni
A M
AM
Sinico
C
C
Schivo
M L
ML
Alhaique
F
F
D000935:Antifungal Agents; D002176:Candida albicans / Q000187:drug effects*; D004337:Drug Carriers; D007654:Ketoconazole / Q000494:pharmacology*; D008825:Miconazole / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D010743:Phospholipids
D000935:Antifungal Agents; D004337:Drug Carriers; D010743:Phospholipids; D008825:Miconazole; D007654:Ketoconazole